- Preparation and characterization of bis[4-dimethylamino-2-pyrimidyl] dichalcogenides (S, Se, Te): X-ray crystal structure of bis[4-dimethylamino-2-pyrimidyl] diselenide and its physicochemical behavior in microemulsion media
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Novel and synthetically important bis[4-dimethylamino-2-pyrimidyl] dichalcogenides (S, Se, Te) have been prepared and characterized with the help of elemental analysis and various spectroscopic techniques. The methodology employs hydrazine hydrate in dimethylformamide to reduce elemental chalcogen to generate the dichalcogenide anions, E22- (E=S, Se, Te), followed by reaction with 2,4-dichloropyrimidine to afford bis[4-dimethylamino-2-pyrimidyl] dichalcogenides in good yield. It further exploits the additional compositional degree of freedom available in mixed surfactant solution to allow solubilization and stabilization of bis[4-dimethylamino-2-pyrimidyl] diselenide in microemulsion media.
- Bhasin,Arora, Ekta,Kaur, Khushwinder,Kang, Sung-Kyu,Gobel, Michael,Klapoetke,Mehta
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Read Online
- Deaminative chlorination of aminoheterocycles
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Selective modification of heteroatom-containing aromatic structures is in high demand as it permits rapid evaluation of molecular complexity in advanced intermediates. Inspired by the selectivity of deaminases in nature, herein we present a simple methodology that enables the NH2 groups in aminoheterocycles to be conceived as masked modification handles. With the aid of a simple pyrylium reagent and a cheap chloride source, C(sp2)?NH2 can be converted into C(sp2)?Cl bonds. The method is characterized by its wide functional group tolerance and substrate scope, allowing the modification of >20 different classes of heteroaromatic motifs (five- and six-membered heterocycles), bearing numerous sensitive motifs. The facile conversion of NH2 into Cl in a late-stage fashion enables practitioners to apply Sandmeyer- and Vilsmeier-type transforms without the burden of explosive and unsafe diazonium salts, stoichiometric transition metals or highly oxidizing and unselective chlorinating agents. [Figure not available: see fulltext.]
- Cornella, Josep,Faber, Teresa,Gómez-Palomino, Alejandro,Ghiazza, Clément
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- Dual targeting of acetylcholinesterase and tau aggregation: Design, synthesis and evaluation of multifunctional deoxyvasicinone analogues for Alzheimer's disease
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Development of multitargeted ligands have demonstrated remarkable efficiency as potential therapeutics for Alzheimer's disease (AD). Herein, we reported a new series of deoxyvasicinone analogues as dual inhibitor of acetylcholinesterase (AChE) and tau aggregation that function as multitargeted ligands for AD. All the multitargeted ligands 11(a-j) and 15(a-g) were designed, synthesized, and validated by 1HNMR, 13CNMR and mass spectrometry. All the synthesized compounds 11(a-j) and 15(a-g) were screened for their ability to inhibit AChE, BACE1, amyloid fibrillation, α-syn aggregation, and tau aggregation. All the screened compounds possessed weak inhibition of BACE-1, Aβ42 and α-syn aggregation. However, several compounds were identified as potential hits in the AChE inhibitory screening assay and cellular tau aggregation screening. Among all compounds, 11f remarkably inhibited AChE activity and cellular tau oligomerization at single-dose screening (10 μM). Moreover, 11f displayed a half-maximal inhibitory concentration (IC50) value of 0.91 ± 0.05 μM and half-maximal effective concentration (EC50) value of 3.83 ± 0.51 μM for the inhibition of AChE and cellular tau oligomerization, respectively. In addition, the neuroprotective effect of 11f was determined in tau-expressing SH-SY5Y cells incubated with Aβ oligomers. These findings highlighted the potential of 11f to function as a multifunctional ligand for the development of promising anti-AD drugs.
- Manzoor, Shoaib,Gabr, Moustafa T.,Rasool, Bisma,Pal, Kavita,Hoda, Nasimul
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- Novel triazole-sulfonamide bearing pyrimidine moieties with carbonic anhydrase inhibitory action: Design, synthesis, computational and enzyme inhibition studies
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A series of new triazole-sulfonamide bearing pyrimidine derivatives were designed and synthesized via click chemistry. All new compounds (SH-1 to SH-28) were validated by 1HNMR, 13CNMR, HRMS, and SH-3 was further structurally validated by X-Ray single diffraction study. These compounds (SH-1 to SH-28) were tested as inhibitors of human carbonic anhydrase (hCA) isoforms, such as hCA I, II, IX and XII, using a stopped flow CO2 hydrase assay. Most of the compounds exhibited significant inhibitory activity against hCA II and weak inhibitory activity against hCA I. The target compounds also displayed moderate to excellent inhibitory activity against tumor-related hCAs IX and XII. Some compounds, e.g., SH-20 (Ki = 9.4 nM), SH-26 (Ki = 1.8 nM) and SH-28 (Ki = 0.82 nM) exhibited excellent inhibitory activity and selectivity profile against hCAs XII over IX. SH-23 displayed promising inhibitory activity and selectivity profile against both tumor-related hCAs IX (Ki = 2.9 nM) as well as XII (Ki = 0.82 nM) over hCA I and II. To understand the molecular interactions, molecular docking study of compounds SH-20, SH-23, SH-26 and SH-28 with hCA XII and SH-23 also with hCA IX were performed. The computational study evidenced favorable interaction between the inhibitors and active residues of both proteins. Some of these derivatives are promising leads for the development of selective, anticancer agents based on CA inhibitors.
- Hoda, Nasimul,Manzoor, Shoaib,Petreni, Andrea,Raza, Md Kausar,Supuran, Claudiu T.
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supporting information
(2021/07/16)
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- Efficient Phosphorus-Free Chlorination of Hydroxy Aza-Arenes and Their Application in One-Pot Pharmaceutical Synthesis
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The chlorination of hydroxy aza-arenes with bis(trichloromethyl) carbonate (BTC) and SOCl2 has been effectively performed by refluxing with 5 wt % 4-dimethylaminopyridine (DMAP) as a catalyst. Various substrates are chlorinated with high yields. The obtained chlorinated aza-arenes can be used directly with simple workup for succedent one-pot synthesis on a large scale.
- Wang, Jian,Li, Yan-Hui,Pan, Song-Cheng,Li, Ming-Fang,Du, Wenting,Yin, Hong,Li, Jing-Hua
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supporting information
p. 146 - 153
(2020/03/10)
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- Preparation method of chloro-substituted polyhydroxy aza-aromatic ring compound (by machine translation)
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The invention discloses a preparation method, namely BTC and SOCl, of a chloropolyhydroxyl aza heteroaromatic ring compound as a raw material with a polyhydroxy aza heteroaromatic ring compound as a raw material, and a preparation method thereof. 2 As the double chlorination reagent, a chloropolyhydroxyl aza-aromatic ring compound is produced by chlorination reaction with 4 - dimethylaminopyridine (DMAP) as a catalyst at room temperature to reflux temperature of the reaction, as a catalyst. BTC TC TC TC2 /DMDMAP chlorination system has high efficiency, high selectivity and chlorine substitution on a polyhydroxy nitrogen heterocyclic compound; the system can replace POCl3 , The production of phosphorus-containing wastewater is avoided. Using BTC as a chlorination reagent, the reaction by-product was HCl and CO. 2 . From the aspects of industrial wastewater treatment, environmental protection and the like, the advantages thereof are obvious; SOCl is distilled off after the reaction is ended. 2 The quantity is almost no loss, can be used repeatedly, and reduces the process cost. (by machine translation)
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Paragraph 0019; 0020
(2019/10/01)
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- Green preparation method of palatinib hydrochloride (by machine translation)
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The invention belongs to the technical field of chemical synthesis of medicines, and belongs to the technical field of pharmaceutical chemistry. The invention particularly relates to a green preparation method. The o-methyl aniline and N - chlorosuccinimide are chlorinated to obtain 2 - methyl -5 - chloro- aniline; the 6 - chlorine - 222H-indole hydrochloride is obtained by reacting with the nitrous acid compound; N-methyl -6 -chloro - 222H-indole; under the participation of dimethyl sulfoxide, 3 - 2-dimethyl 3 - chlorine -6 - 222H-indazole; and the like. A reaction with 2 - chloro -4 - amino - pyrimidine and iodomethane gave N - (2 -chloropyrimidine -4 -yl) - N N-methyl -2, 3 -dimethyl - 222H-indazole -6 - amine; and finally, a pimatinib hydrochloride salt was obtained by reaction with 3 - sulfanilide -4 - methyl - aniline. The method is low in raw material price, simple to operate, low in operation risk, capable of avoiding waste acid generation, high in reaction yield, and high in purity. (by machine translation)
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Paragraph 0077-0085
(2019/08/01)
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- Preparation method for 2,4-dichloropyrimidine and derivatives thereof
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The invention discloses a preparation method for 2,4-dichloropyrimidine and derivatives thereof. A catalyst, a compound 1 and phosgene are involved in the preparation method. The compound 1 reacts with the phosgene under the action of the catalyst in a solvent. The preparation method is reasonably designed, is convenient for use and is capable of solving the problems of high discharge of phosphorus wastewater and environmental pollution of the traditional process; the end product prepared according to the method is high in conversion rate, the preparation period is short and the problem of environmental pollution is reduced; the method is energy-saving and environment-friendly and is suitable for extensive promotion.
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Paragraph 0043; 0044
(2019/04/14)
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- Preparation method of pharmaceutical intermediate 2,4-dichloro-5-pyrimidine formaldehyde
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The invention discloses a preparation method of a pharmaceutical intermediate 2,4-dichloro-5-pyrimidine formaldehyde, and belongs to the technical field of pharmaceutical synthesis. According to the key point of the technical scheme, the preparation method comprises the steps: uracil is used as a starting material, Vilsmeier-Haack reaction is carried out at low temperature and aldehyde groups arenot subjected to chlorination reaction under protection of a protective agent aluminum trichloride or boric acid, then heating is carried out, and chlorination reaction is carried out with phosphorusoxychloride to generate the target product pharmaceutical intermediate 2,4-dichloro-5-pyrimidine formaldehyde. The preparation method has the advantages of mild reaction conditions, high yield and good product purity, and is a synthetic method with industrial production value.
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Paragraph 0014; 0015
(2018/09/26)
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- Quinoline-pyrimidine hybrids: Synthesis, antiplasmodial activity, SAR, and mode of action studies
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For the treatment of malaria which affects nearly 200 million people each year and the continued exacerbation by the emergence of drug resistance to most of the available antimalarials, the "covalent bitherapy" suggests hybrid molecules to be the next-generation antimalarial drugs. In this investigation, new hybrids of 4-aminoquinoline and pyrimidine moieties that show antiplasmodial activity in the nM range against chloroquine-resistant as well as chloroquine-sensitive strains of Plasmodium falciparum have been prepared. Cytotoxicity evaluation and mode of action of most potent hybrid molecule have been conducted.
- Singh, Kamaljit,Kaur, Hardeep,Smith, Peter,De Kock, Carmen,Chibale, Kelly,Balzarini, Jan
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p. 435 - 448
(2014/02/14)
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- Novel Hinge-Binding Motifs for Janus Kinase 3 Inhibitors: A Comprehensive Structure-Activity Relationship Study on Tofacitinib Bioisosteres
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The Janus kinases (JAKs) are a family of cytosolic tyrosine kinases crucially involved in cytokine signaling. JAKs have been demonstrated to be valid targets in the treatment of inflammatory and myeloproliferative disorders, and two inhibitors, tofacitinib and ruxolitinib, recently received their marketing authorization. Despite this success, selectivity within the JAK family remains a major issue. Both approved compounds share a common 7H-pyrrolo[2,3-d]pyrimidine hinge binding motif, and little is known about modifications tolerated at this heterocyclic core. In the current study, a library of tofacitinib bioisosteres was prepared and tested against JAK3. The compounds possessed the tofacitinib piperidinyl side chain, whereas the hinge binding motif was replaced by a variety of heterocycles mimicking its pharmacophore. In view of the promising expectations obtained from molecular modeling, most of the compounds proved to be poorly active. However, strategies for restoring activity within this series of novel chemotypes were discovered and crucial structure-activity relationships were deduced. The compounds presented may serve as starting point for developing novel JAK inhibitors and as a valuable training set for in silico models.
- Gehringer, Matthias,Forster, Michael,Pfaffenrot, Ellen,Bauer, Silke M.,Laufer, Stefan A.
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supporting information
p. 2516 - 2527
(2015/08/24)
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- Synthesis of new organochalcogen (Se or Te) based multifunctional pyrimidine derivatives: X-ray structure determination of 2,4- bis(arylchalcogenyl)pyrimidine and 2-chloro-4,6-bis(arylchalcogenyl)pyrimidine compounds
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A new class of multinucleate pyrimidine chalcogen (Se/Te) derivatives, i.e. 2,4-bis(arylchalcogenyl)pyrimidine and 2-chloro-4,6-bis(arylchalcogenyl) pyrimidine compounds, has been synthesized for the first time by the nucleophilic substitution of chlorine at the C-2 and C-4 positions of 2,4-dichloropyrimidine and at the C-4 and C-6 positions of 2,4,6- trichloropyrimidine with a variety of chalcogen bearing aryl anions ArE - (Ar = phenyl, 1-naphthyl, p-tolyl). All the newly prepared pyrimidyl chalcogen compounds have been thoroughly characterized with the help of various spectroscopic techniques, viz, NMR (1H, 13C, 77Se), FT-IR and mass spectrometry (in representative cases). The crystal structures of 2,4-bis(naphthalen-1-ylselanyl)pyrimidine (1c), 2,4-bis(phenyltelluryl)pyrimidine (1d), 2-chloro-4,6-bis(phenylselanyl) pyrimidine (2a) and 4,6-bis(p-tolylselanyl)-2-chloropyrimidine (2b) were confirmed by X-ray crystallographic analysis.
- Arora, Ekta,Bhasin,Mehta,Sharma, Nidhi,Bhasin,Jacob, Claus,Félix, Vítor,Neogi, Subhadip
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p. 316 - 322
(2014/08/05)
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- PROCESS FOR RILPIVIRINE
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The present invention provides a novel process for the preparation of 4-(4-hydroxypyrimidin-2-ylamino)benzonitrile. The present invention also provides a novel process for the preparation of 4-iodo-2,6-dimethyl benzenamine. The present invention further provides an improved process for the preparation of rilpivirine. The present invention further provides a tosylate salt of rilpivirine, process for its preparation and pharmaceutical compositions comprising it.
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Paragraph 0078
(2014/08/19)
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- RILPIVIRINE HYDROCHLORIDE
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The present invention provides a novel process for the preparation of rilpivirine. The present invention also provides a novel process for the preparation of rilpivirine hydrochloride. The present invention further provides a rilpivirine hydrochloride monohydrate, process for its preparation and pharmaceutical compositions comprising it.
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Paragraph 0080; 0081
(2014/12/09)
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- RILPIVIRINE HYDROCHLORIDE
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As used herein the term "room temperature" refers to a temperature of about 25°C to about 35°C. According to one aspect of the present invention, there IS provided a novel process for the preparation of rilpivirine, which comprises: a) condensing the (E)-3-( 4-amino-3,5-dimethylphenyl)acrylonitrile hydrochloride with 4-( 4-chloropyrimidin-2-ylamino )benzonitrile m the presence of Nmethylpyrrolidone; b) heating the contents obtained in step (a) at about 75 to 95°C to obtain a solution; c) cooling the solution obtained in step (b) at below 35°C; d) adding water to the reaction mass; and e) isolating rilpivirine. The reaction in step (b) may preferably be heated to 100 to 110°C. Step (c) may preferably be carried out at room temperature. Rilpivirine may be isolated in step (e) by the methods known such as Filtration or centrifugation.
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Page/Page column 7; 8
(2013/03/28)
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- Development of two scalable syntheses of 4-amino-5-aminomethyl-2- methylpyrimidine: Key intermediate for vitamin b1
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Two scalable processes for the synthesis of 4-amino-5-aminomethyl-2- methylpyrimidine (2) are described. In the first approach, the less expensive 2-cyanoacetamide was reacted with Vilsmeier reagent to afford enamine 18, followed by the condensation with acetamidine to produce the 4-amino-2-methylpyrimidine-5-carbonitrile (6); subsequent hydrogenation gave 2 in 65% overall yield. In the second approach, malononitrile was treated with the ionic salt 21, prepared in situ from DMF and dimethyl sulfate, to give 18, which, without isolation was reacted with acetamidine hydrochloride to afford the common intermediate 6. Overall yield of this approach was 70%. Both methods are performed in a convenient manner suitable for industrial use.
- Zhao, Lei,Ma, Xiao-Dong,Chen, Fen-Er
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body text
p. 57 - 60
(2012/05/31)
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- Tetrapodal amidoxime ligands I. Coordination isomerism due to self-complementary dimerization of a pyramidal cobalt(iii) coordination module
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A bis-μ-amidoximato-bridged cobalt(iii) dimer obtained with a new tetrapodal ligand possesses interesting structural parameters as a consequence of intramolecular hydrogen bonding intentionally built into the complex. Its synthesis and properties are described. The new ligand type combines attributes of two previously described ligand classes: It binds a metal ion in a tetrapodal pentadentate fashion and forms a pseudomacrocycle through hydrogen bonds, characteristic of chelating oxime ligands. Coordination isomerism, which is a consequence of dimer formation, has been analyzed by means of X-ray crystallography and carbon-13 nuclear magnetic resonance spectroscopy. The Royal Society of Chemistry 2012.
- Boyd, John P.,Irran, Elisabeth,Grohmann, Andreas
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experimental part
p. 2477 - 2485
(2012/03/22)
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- PROCESS FOR RILPIVIRINE
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The present invention provides a novel process for the preparation of 4-(4-hydroxypyrimidin-2-ylamino)benzonitrile. The present invention also provides a novel process for the preparation of 4-iodo-2,6-dimethyl benzenamine. The present invention further provides an improved process for the preparation of rilpivirine. The present invention further provides a tosylate salt of rilpivirine, process for its preparation and pharmaceutical compositions comprising it.
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Page/Page column 7
(2012/11/13)
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- Phosphonium chloride as a non-volatile chlorinating reagent: Preparation and reaction in no solvent or ionic liquid
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Reaction of triphenylphosphine with trichloroisocyanuric acid in no solvent or an ionic liquid gave the corresponding phosphonium chloride, which can be used as a cheap and safe chlorinating reagent. Conversion of hydroxyheterocycles to chloroheterocycles, carboxylic acids to carboxylic acid chlorides, and primary amides to nitriles were accomplished by using the phosphonium chloride in excellent to good yields.
- Sugimoto, Osamu,Harada, Yukihiro,Tanji, Ken-Ichi
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p. 1583 - 1590
(2013/08/15)
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- Solvent-free or low-solvent large-scale preparation of chloropyrimidine and analogues
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Chloropyrimidine or other N-containing aromatic heterocyclic analogues can be efficiently prepared from the corresponding hydroxylated precursors under solvent-free or low-solvent conditions with equimolar or less chlorinating reagents. This high-yielding protocol allows successful preparations of multigram and kilogram batches of these important synthetic intermediates.
- Sun, Zhihua,Wang, Han,Wen, Kun,Li, Ya,Fan, Erkang
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experimental part
p. 4149 - 4153
(2011/07/07)
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- The efficient one-step chlorination of methylsulfanyl group on pyrimidine ring system with sulfuryl chloride
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A facile one-step transformation of methylsulfanyl and arylsulfanyl groups on pyrimidine ring system into the corresponding chloride group was achieved using sulfuryl chloride in acetonitrile/dichloromethane.
- Ham, Young Jin,Lee, Duck-Hyung,Choi, Hwan Geun,Hah, Jung-Mi,Sim, Taebo
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experimental part
p. 4609 - 4611
(2010/09/18)
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- A novel approach toward the synthesis and characterization of pyrimidyl chalcogen compounds
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A variety of hitherto unknown symmetrical and unsymmetrical pyrimidyl chalcogen compounds have been synthesized and characterized by elemental analysis using various spectroscopic techniques viz. NMR 1H, 13C, 77Se and infrared. Two different methodologies were employed. The first method involves the use of hydrazine hydrate as reducing agent to generate dichalcogenide anions followed by reaction with 2, 4-dichloropyrimidine to give the dichalcogenide compounds in good yield. The second method employs chlorine-magnesium exchange of 2,4-dichloropyrimidine using iso propyl magnesium chloride. The synthesis of the mixed phenyl pyrimidyl selenides have been achieved using sodium borohydride in ethanol as a reductive reagent to cleave Se-Se bond followed by alkylation with 2-chloro-4, 6-dimethylpyrimidine and 2, 4-dichloropyrimidine.
- Bhasin,Arora, Ekta,Rishu,Doomra, Shivani,Nishima,Nagpal, Yogesh,Kumar, Rajeev,Weigand,Mehta
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body text
p. 986 - 991
(2009/04/06)
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- Methods of using pyrimidine-based antiviral agents
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The invention provides novel methods of using substituted pyrimidine compounds and compositions for the treatment or prevention of diseases associated with CMV infection. In particular, the present invention provides methods for the treatment or prevention of cardiovascular diseases and organ transplant rejection.
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- Arylsulfonic acid salts of pyrimidine-based antiviral
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Salts of pyrimidine derivatives are provided having the formula: wherein R represents hydrogen, methyl or ethyl; Z represents a substituted or unsubstituted 1-piperidinyl, a substituted or unsubstituted 4-morpholinyl, or a substituted or unsubstituted 1-pyrrolidinyl; and Ar represents a substituted or unsubstituted phenyl or a substituted or unsubstituted naphthyl. These salts are particularly useful as antiviral agents (e.g., to treat CMV infections).
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- Alpha-substituted pyrimidine-thioalkyl and alkylether compounds as inhibitors of viral reverse transcriptase
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The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R 4 is selected from the group consisitng of --H or --NR 15 R 16 where R 15 is --H and R 16 is --H, C 1 -C 6 alkyl, NH 2 or R 15 and R 16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R 6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R 4 and R 6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive being inhibitors of viral reverse transcriptase. STR1
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- Pyrimidine-thioalkyl and alkylether compounds
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The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R 4 is selected from the group consisting of --H or --NR 15 R 16 where R 15 is --H and R 16 is --H, C 1 -C 6 alkyl, --NH 2 or R 15 and R 16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R 6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R 4 and R 6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive.
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- Stereocontrolled synthesis of β-2'-deoxypyrimidine nucleosides via intramolecular glycosylations
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A pyrimidine moiety was tethered at the 3'-β-position of D-threo-furanosides. By carefully controlling the reaction conditions, pyrimidine bases can be delivered to the anomeric center to give of β-pyrimidine nucleosides in good yield and with complete stereocontrol.
- Xia, Xiaoyang,Wang, Jianying,Hager, Michael W.,Sisti, Nicholas,Liotta, Dennis C.
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p. 1111 - 1114
(2007/10/03)
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- Process for the preparation of chloropyrimidines
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A process for the preparation of chloropyrimidines of the formula STR1 in which the substituents may be alkyl, cycloalkyl, aryl or radicals containing heteroatoms, but in which at least one of the substituents R1 to R4 must be Cl, which involves: reacting a hydroxy-pyrimidine or its tautomeric keto form with phosphoryl chloride in the presence of an amine or amine hydrochloride; recovering phosphoryl chloride after the reaction by adding phosphorus pentachloride and distilling the phosphoryl chloride; and separating the chloropyrimidine from the amine hydrochloride by addition of a solvent which will dissolve the chloropyrimidine but not the amine hydrochloride and removing the amine hydrochloride.
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- Herbicidal sulfonylurea derivatives
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The invention embraces compounds of formula STR1 and salts thereof, wherein: X and Y are independently selected from various optionally substituted alkoxy, alkenyloxy, alkynyoxy and phenoxy groups; W is oxygen or sulfur; R1 is hydrogen or alkyl; E is CH or N; R2 and R3 are independently selected from various halo, alkyl, alkoxy and amino substituents. The compounds of the invention show herbicidal properties particularly for the control of broad leaf plants in grass crops such as wheat. In further embodiments the invention provides processes for the preparation of compounds I, intermediates useful in the preparation of compounds of formula I, compositions containing as active ingredient a compound of formula I and herbicidal and plant growth regulating processes utilizing compounds of formula I.
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- Flame-resistant polycarbonates containing units deriving from halogenated pyrimidine compounds in their polymer chain
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Flame-resistant thermoplastic branched polycarbonates of high molecular weight are prepared from: (1) a carbonate precursor; (2) at least one dihydroxyaromatic compound of formula: where:, R is a single bond, or a substituted or non-substituted linear or branched C1-C5 alkylene radical, or a group chosen from O, S, SO2 and CO;, X and Y, which may be the same or different, are H or CH3;, m and n, which may be the same or different, are whole numbers from 1 to 4; (3) at last one halogenated pyrimidine compound of formula: where: R2, R3, R4, which may be the same or different, are chlorine or bromine or hydrogen, on condition that at least one is chlorine or bromine;, R1 is chlorine or bromine, or a radical of formula: where Z is NH or S or O; (4) at least one polyfunctional organic compound as branching agent, characterized by possessing at least three equal or different groups chosen from the groups OH, COOH, COCl and SO2Cl.
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- Herbicidal sulfonylurea derivatives
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The invention embraces compounds of formula and salts thereof, wherein:, , X and Y are independently selected from various optionally substituted alkoxy, alkenyloxy, alkynyoxy and phenoxy groups;, W is oxygen or sulfur;, R1 is hydrogen or alkyl;, E is CH or N;, R2 and R3 are independently selected from various halo, alkyl, alkoxy and amino substituents. The compounds of the invention show herbicidal properties particularly for the control of broad leaf plants in grass crops such as wheat. In further embodiments the invention provides processes for the preparation of compounds I, intermediates useful in the preparation of compounds of formula I, compositions containing as active ingredient a compound of formula I and herbicidal and plant growth regulating processes utilizing compounds of formula I.
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- The anti-H1-histaminic and antimuscarinic effect of 2- and 4-[benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds
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This paper reports the synthesis of 2- and 4- [benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds and the evaluation of their inhibitory properties against histamine (H1), acetylcholine and barium chloride, on guinea pig isolated ileum. 4-[p.Methoxybenzyl-(2-dimethylaminoethyl)amino]-2-methoxy-pyrimidine (VIII) is shown to possess H1 receptor antagonist activity, with a potency similar to that observed for Tonzylamine. By contrast, a specific, although weak, antimuscarinic effect is displayed by 4-[benzyl-(2-dimethylaminoethyl)amino]-2-methoxy-5-methylthio-pyrimidine (XII).
- Maggiali,Morini,Mossini,Morini,Barocelli,Impicciatore
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p. 277 - 291
(2007/10/02)
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